1199-34-4Relevant academic research and scientific papers
Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure-Activity Relationship, Metabolism, and Biology Triaging
Van Der Westhuyzen, Renier,Mabhula, Amanda,Njaria, Paul M.,Müller, Rudolf,Ngumbu Muhunga, Denis,Taylor, Dale,Lawrence, Nina,Njoroge, Mathew,Brunschwig, Christel,Moosa, Atica,Singh, Vinayak,Rao, Srinivasa P.S.,Manjunatha, Ujjini H.,Smith, Paul W.,Warner, Digby F.,Street, Leslie J.,Chibale, Kelly
, p. 9444 - 9457 (2021/07/19)
Screening of a library of small polar molecules against Mycobacterium tuberculosis (Mtb) led to the identification of a potent benzoheterocyclic oxime carbamate hit series. This series was subjected to medicinal chemistry progression underpinned by structure-activity relationship studies toward identifying a compound for proof-of-concept studies and defining a lead optimization strategy. Carbamate and free oxime frontrunner compounds with good stability in liver microsomes and no hERG channel inhibition liability were identified and evaluated in vivo for pharmacokinetic properties. Mtb-mediated permeation and metabolism studies revealed that the carbamates were acting as prodrugs. Toward mechanism of action elucidation, selected compounds were tested in biology triage assays to assess their activity against known promiscuous targets. Taken together, these data suggest a novel yet unknown mode of action for these antitubercular hits.
Benzothiazole-oxazole type alpha-glucosidase inhibitor and preparation method and application thereof
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Paragraph 0022; 0023, (2018/10/19)
The invention discloses a benzothiazole-oxazole type alpha-glucosidase inhibitor and a preparation method and application thereof. The method comprises the following steps: adding a compound (II) andhydroxylamine hydrochloride in a methanol aqueous solution and a sodium carbonate aqueous solution to obtain a compound (III); adding the compound (III), zinc powder and ammonium formate in methanol and reacting to obtain a compound (IV); and adding the compound (IV), a compound (V), iodine and potassium carbonate in DMF and reacting to obtain a compound (I). The chemical formula of the compound (I) is as shown in specification, the chemical formula of the compound (II) is as shown in specification, the chemical formula of the compound (III) is as shown in specification, the chemical formula of the compound (IV) is as shown in specification, and the chemical formula of the compound (V) is as shown in specification. The benzothiazole-oxazole type compound has obvious inhibition effect on alpha-glucosidase, the preparation method is simple, reaction conditions are gentle, and thus, the benzothiazole-oxazole type alpha-glucosidase inhibitor is suitable for being industrially produced on alarge scale.
Glucose-derived spiro-isoxazolines are anti-hyperglycemic agents against type 2 diabetes through glycogen phosphorylase inhibition
Goyard, David,Kónya, Bálint,Chajistamatiou, Aikaterini S.,Chrysina, Evangelia D.,Leroy, Jérémy,Balzarin, Sophie,Tournier, Michel,Tousch, Didier,Petit, Pierre,Duret, Cédric,Maurel, Patrick,Somsák, László,Docsa, Tibor,Gergely, Pál,Praly, Jean-Pierre,Azay-Milhau, Jacqueline,Vidal, Sébastien
supporting information, p. 444 - 454 (2015/12/24)
Glycogen phosphorylase (GP) is a target for the treatment of hyperglycaemia in the context of type 2 diabetes. This enzyme is responsible for the depolymerization of glycogen into glucose thereby affecting the levels of glucose in the blood stream. Twelve
SPIRO-OXADIAZOLINE COMPOUNDS AS AGONISTS OF α-7-NICOTINIC ACETYLCHOLINE RECEPTORS
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Paragraph 00212-00213, (2015/05/19)
The present invention relates to novel spiro-oxadiazoline compounds that are suitable as agonists or partial agonists of a7-nAChR, and pharmaceutical compositions of the same, methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering a spiro-oxadiazoline cx7-nAChR agonist or partial agonist, to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
